Synthesis of macrocyclic ketones exploiting palladium-catalyzed activation of carboxylic acids as an enabling step

Abstract

The novel synthesis of macrocyclic arylketones via palladium-catalyzed cross-coupling of arylboronic acids and carboxylic acids, activated by the treatment with di(N-succinimidyl) carbonate, is disclosed. This allows the high yielding synthesis of various functionalized arylketones, which can be converted into macrocycles via a Mitsunobu protocol.